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Chemical Structure : TPA023
Catalog No.: PC-62769Not For Human Use, Lab Use Only.
TPA023 is a potent, α2/α3 subtype-selective, and oral GABAA receptor agonist with Kd of 0.92, 1.05 and 0.58 nM for α1-, α2-, α3-, and α5-containing human receptors.
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TPA023 (MK-0777) is a potent, α2/α3 subtype-selective, and oral GABAA receptor agonist with Kd of 0.92, 1.05 and 0.58 nM for α1-, α2-, α3-, and α5-containing human receptors.
TPA023 (MK-0777) shows much lower (50- to 2000-fold) affinities for α4 and α6 subtypes (Ki= 60 and 418 nM, respectively).
TPA023 (MK-0777) demonstrates anxiolytic-like efficacy and anticonvulsant activity in mouse pentylenetetrazole seizure model.
| M.Wt | 395.442 | |
| Formula | C20H22FN7O | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Atack JR, et al. J Pharmacol Exp Ther. 2010 Jan;332(1):17-25.
2. de Haas SL, et al. J Psychopharmacol. 2007 Jun;21(4):374-83.
3. Carling RW, et al. J Med Chem. 2005 Nov 17;48(23):7089-92.
4. Atack JR, et al. J Pharmacol Exp Ther. 2006 Jan;316(1):410-22.
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